Structured Review

GE Healthcare h cgp 12177
Inhibition of  3 H-CGP 12177-specific binding in whole CHO cells expressing human β1-adrenoceptor ( A ) and human β2-adrenoceptor ( B ). Nonspecific binding was determined by 10 μM propranolol. Concentration of  3 H-CGP 12177 present was 0.97 nM ( A ) and 1.11 nM ( B ). Data points are means ±  se  of triplicate determinations. Results of single experiments shown are representative of 8 separate experiments in each case.
H Cgp 12177, supplied by GE Healthcare, used in various techniques. Bioz Stars score: 86/100, based on 2 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/result/h cgp 12177/product/GE Healthcare
Average 86 stars, based on 2 article reviews
Price from $9.99 to $1999.99
h cgp 12177 - by Bioz Stars, 2020-04
86/100 stars

Images

1) Product Images from "Predicting in vivo cardiovascular properties of ?-blockers from cellular assays: a quantitative comparison of cellular and cardiovascular pharmacological responses"

Article Title: Predicting in vivo cardiovascular properties of ?-blockers from cellular assays: a quantitative comparison of cellular and cardiovascular pharmacological responses

Journal: The FASEB Journal

doi: 10.1096/fj.11-192435

Inhibition of  3 H-CGP 12177-specific binding in whole CHO cells expressing human β1-adrenoceptor ( A ) and human β2-adrenoceptor ( B ). Nonspecific binding was determined by 10 μM propranolol. Concentration of  3 H-CGP 12177 present was 0.97 nM ( A ) and 1.11 nM ( B ). Data points are means ±  se  of triplicate determinations. Results of single experiments shown are representative of 8 separate experiments in each case.
Figure Legend Snippet: Inhibition of 3 H-CGP 12177-specific binding in whole CHO cells expressing human β1-adrenoceptor ( A ) and human β2-adrenoceptor ( B ). Nonspecific binding was determined by 10 μM propranolol. Concentration of 3 H-CGP 12177 present was 0.97 nM ( A ) and 1.11 nM ( B ). Data points are means ± se of triplicate determinations. Results of single experiments shown are representative of 8 separate experiments in each case.

Techniques Used: Inhibition, Binding Assay, Expressing, Concentration Assay

2) Product Images from "Impact of Polymorphic Variants on the Molecular Pharmacology of the Two-Agonist Conformations of the Human ?1-Adrenoceptor"

Article Title: Impact of Polymorphic Variants on the Molecular Pharmacology of the Two-Agonist Conformations of the Human ?1-Adrenoceptor

Journal: PLoS ONE

doi: 10.1371/journal.pone.0077582

The effect of pre-incubation with pertussis toxin on 3 H-cAMP accumulation responses. 3 H-cAMP accumulation in A CHO cells expressing the human adenosine A1 receptor, B and E wildtype β1-adrenoceptor cells, C and F Gly49/Gly389 cells and D and G Ser49/Arg389 cells. All cells were subjected to 24 hours in serum free media before experimentations, those with closed circles in the absence of PTX and those with open circles in the presence of PTX. Bars represent A basal 3 H-cAMP accumulation and that in response to 10 µM forskolin, B–G basal 3 H-cAMP accumulation and that in response to 10 µM isoprenaline following incubation in serum free media without and with PTX. Data points are mean ± s.e.mean of triplicate determinations and these single experiments are representative of 4 separate experiments in each case. A demonstrates that the PTX pre-incubation was successfully preventing the Gi-coupled responses to cyclopentyladenosine (CPA) in CHO cells expressing the human A1 adenosine receptor, however there was no effect of PTX pre-incubation on the cimaterol (catecholamines conformation) or CGP 12177 (secondary conformation) responses occurring via the wildtype human β1-adrenoceptor or the polymorphic variants.
Figure Legend Snippet: The effect of pre-incubation with pertussis toxin on 3 H-cAMP accumulation responses. 3 H-cAMP accumulation in A CHO cells expressing the human adenosine A1 receptor, B and E wildtype β1-adrenoceptor cells, C and F Gly49/Gly389 cells and D and G Ser49/Arg389 cells. All cells were subjected to 24 hours in serum free media before experimentations, those with closed circles in the absence of PTX and those with open circles in the presence of PTX. Bars represent A basal 3 H-cAMP accumulation and that in response to 10 µM forskolin, B–G basal 3 H-cAMP accumulation and that in response to 10 µM isoprenaline following incubation in serum free media without and with PTX. Data points are mean ± s.e.mean of triplicate determinations and these single experiments are representative of 4 separate experiments in each case. A demonstrates that the PTX pre-incubation was successfully preventing the Gi-coupled responses to cyclopentyladenosine (CPA) in CHO cells expressing the human A1 adenosine receptor, however there was no effect of PTX pre-incubation on the cimaterol (catecholamines conformation) or CGP 12177 (secondary conformation) responses occurring via the wildtype human β1-adrenoceptor or the polymorphic variants.

Techniques Used: Incubation, Expressing

Inhibition of cimaterol-induced 3 H-cAMP accumulation responses by CGP 12177. 3 H-cAMP accumulation in response to cimaterol in A wildtype cells, B Gly49/Gly389 cells and C Ser49/Arg389 cells in the absence and presence of CGP 12177. Bars represent basal 3 H-cAMP accumulation, that in response to 10 µM isoprenaline and that in response to 1 nM and 10 nM CGP 12177. Data points are mean ± s.e.mean of triplicate determinations and these single experiments are representative of 4 separate experiments in each case. Here, CGP 12177 inhibits the catecholamine conformation response with high affinity in all three receptor variants.
Figure Legend Snippet: Inhibition of cimaterol-induced 3 H-cAMP accumulation responses by CGP 12177. 3 H-cAMP accumulation in response to cimaterol in A wildtype cells, B Gly49/Gly389 cells and C Ser49/Arg389 cells in the absence and presence of CGP 12177. Bars represent basal 3 H-cAMP accumulation, that in response to 10 µM isoprenaline and that in response to 1 nM and 10 nM CGP 12177. Data points are mean ± s.e.mean of triplicate determinations and these single experiments are representative of 4 separate experiments in each case. Here, CGP 12177 inhibits the catecholamine conformation response with high affinity in all three receptor variants.

Techniques Used: Inhibition

Inhibition of 3 H-cAMP accumulation responses to cimaterol and CGP 12177 at the wildtype and polymorphic variant receptors. 3 H-cAMP accumulation in response to cimaterol and CGP 12177 in A and D wildtype (WT) cells, B and E Gly49/Gly389 cells and C and F Ser49/Arg389 cells in the absence and presence of bisoprolol and carvedilol. Bars represent basal 3 H-cAMP accumulation, that in response to 10 µM isoprenaline and that in response to 30 nM bisoprolol or 3 nM carvedilol for A , B and C or 10 µM bisoprolol or 1 µM carvedilol for D , E and F . Data points are mean ± s.e.mean of triplicate determinations and these single experiments are representative of 4 separate experiments in each case. This demonstrates the difference in the affinity of antagonists for the catecholamine (high affinity) conformation and secondary (low affinity) conformation of the receptors and that both of these conformations exist in all receptor variants.
Figure Legend Snippet: Inhibition of 3 H-cAMP accumulation responses to cimaterol and CGP 12177 at the wildtype and polymorphic variant receptors. 3 H-cAMP accumulation in response to cimaterol and CGP 12177 in A and D wildtype (WT) cells, B and E Gly49/Gly389 cells and C and F Ser49/Arg389 cells in the absence and presence of bisoprolol and carvedilol. Bars represent basal 3 H-cAMP accumulation, that in response to 10 µM isoprenaline and that in response to 30 nM bisoprolol or 3 nM carvedilol for A , B and C or 10 µM bisoprolol or 1 µM carvedilol for D , E and F . Data points are mean ± s.e.mean of triplicate determinations and these single experiments are representative of 4 separate experiments in each case. This demonstrates the difference in the affinity of antagonists for the catecholamine (high affinity) conformation and secondary (low affinity) conformation of the receptors and that both of these conformations exist in all receptor variants.

Techniques Used: Inhibition, Variant Assay

Demonstration of two agonist conformations of the wildtype β1-adrenoceptor and polymorphic variants. 3 H-cAMP accumulation in response to CGP 12177 in A wildtype cells, B Gly49/Gly389 cells and C Ser49/Arg389 cells in the absence and presence of 30 nM cimaterol. Bars represent basal 3 H-cAMP accumulation, that in response to 10 µM isoprenaline and that in response to 30 nM cimaterol. Data points are mean ± s.e.mean of triplicate determinations and these single experiments are representative of 5 separate experiments in each case. Low concentrations of CGP 12177 inhibit the high affinity catecholamine conformation and higher concentrations of CGP 12177 stimulate an agonist response. This demonstrates the two agonist conformations of the wildtype β1-adrenoceptor and that both of these agonist conformations are present in both polymorphic variants.
Figure Legend Snippet: Demonstration of two agonist conformations of the wildtype β1-adrenoceptor and polymorphic variants. 3 H-cAMP accumulation in response to CGP 12177 in A wildtype cells, B Gly49/Gly389 cells and C Ser49/Arg389 cells in the absence and presence of 30 nM cimaterol. Bars represent basal 3 H-cAMP accumulation, that in response to 10 µM isoprenaline and that in response to 30 nM cimaterol. Data points are mean ± s.e.mean of triplicate determinations and these single experiments are representative of 5 separate experiments in each case. Low concentrations of CGP 12177 inhibit the high affinity catecholamine conformation and higher concentrations of CGP 12177 stimulate an agonist response. This demonstrates the two agonist conformations of the wildtype β1-adrenoceptor and that both of these agonist conformations are present in both polymorphic variants.

Techniques Used:

Inhibition of  3 H-CGP 12177 binding at the wildtype receptor and polymorphic variants. Inhibition of  3 H-CGP 12177 specific binding by  A  metoprolol and  B  carvedilol in wildtype (WT), Gly49/Gly389 cells and Ser49/Arg389 cells. Non-specific binding was determined by 10 µM propranolol. The concentration of  3 H-CGP 12177 present in each case was 0.96 nM. Data points are mean ± s.e.mean of triplicate determinations and these single experiments are representative of 6 separate experiments in each case.  C  Correlation plot for the affinity of all the ligands from   Table 1  for the wildtype (x-axis) and polymorphic variants (y-axis). There is a strong correlation between the affinity measurements made in the wildtype and those measured in either the Gly49/Gly389 receptor (R 2  = 1.00, slope 0.99±0.01) and the Ser49/Arg389 receptor (R 2  = 0.99, slope = 0.92±0.02). This demonstrates that ligands had very similar affinity for all three receptors.
Figure Legend Snippet: Inhibition of 3 H-CGP 12177 binding at the wildtype receptor and polymorphic variants. Inhibition of 3 H-CGP 12177 specific binding by A metoprolol and B carvedilol in wildtype (WT), Gly49/Gly389 cells and Ser49/Arg389 cells. Non-specific binding was determined by 10 µM propranolol. The concentration of 3 H-CGP 12177 present in each case was 0.96 nM. Data points are mean ± s.e.mean of triplicate determinations and these single experiments are representative of 6 separate experiments in each case. C Correlation plot for the affinity of all the ligands from Table 1 for the wildtype (x-axis) and polymorphic variants (y-axis). There is a strong correlation between the affinity measurements made in the wildtype and those measured in either the Gly49/Gly389 receptor (R 2  = 1.00, slope 0.99±0.01) and the Ser49/Arg389 receptor (R 2  = 0.99, slope = 0.92±0.02). This demonstrates that ligands had very similar affinity for all three receptors.

Techniques Used: Inhibition, Binding Assay, Concentration Assay

3) Product Images from "Pharmacological characterization of CGP 12177 at the human ?2-adrenoceptor"

Article Title: Pharmacological characterization of CGP 12177 at the human ?2-adrenoceptor

Journal: British Journal of Pharmacology

doi: 10.1038/sj.bjp.0704855

3 H-cyclic AMP accumulation in response to isoprenaline and CGP 12177. The bar represents basal  3 H-cAMP accumulation. Data points are quadruplicate mean±s.e.mean from a single experiment and this is representative of three separate experiments.
Figure Legend Snippet: 3 H-cyclic AMP accumulation in response to isoprenaline and CGP 12177. The bar represents basal 3 H-cAMP accumulation. Data points are quadruplicate mean±s.e.mean from a single experiment and this is representative of three separate experiments.

Techniques Used:

4) Product Images from "ADP-Ribosylation Factors Modulate the Cell Surface Transport of G Protein-Coupled Receptors S⃞"

Article Title: ADP-Ribosylation Factors Modulate the Cell Surface Transport of G Protein-Coupled Receptors S⃞

Journal: The Journal of Pharmacology and Experimental Therapeutics

doi: 10.1124/jpet.109.161489

Inhibition of the cell surface expression of α 2B -AR, β 2 -AR, AT1R, and CXCR4 by BFA treatment. A, the cell surface expression of the receptors in cells treated with BFA. HEK293 cells were transfected with α 2B -AR-GFP, β 2 -AR-GFP, AT1R-GFP, or HA-CXCR4 and treated with BFA at a concentration of 5 μg/ml for 8 h. The cell surface expression of α 2B -AR, β 2 -AR, and AT1R was determined by intact cell ligand binding using [ 3 H]RX 821002, [ 3 H]CGP-12177, and 125 I-Ang II, respectively, as described under Materials and Methods . The mean values of specific ligand binding were 22,737 ± 714, 17,718 ± 771, and 16,754 ± 782 ( n = 3, each in triplicate) from cells transfected with α 2B -AR, β 2 -AR, and AT1R, respectively. The cell surface expression of HA-CXCR4 was measured by flow cytometry after staining with anti-HA antibodies in unpermeabilized cells. The data shown are percentages of the mean value obtained from cells transfected with individual receptor and treated with ethanol (control) and are presented as the mean ± S.E. of three experiments. ∗, P
Figure Legend Snippet: Inhibition of the cell surface expression of α 2B -AR, β 2 -AR, AT1R, and CXCR4 by BFA treatment. A, the cell surface expression of the receptors in cells treated with BFA. HEK293 cells were transfected with α 2B -AR-GFP, β 2 -AR-GFP, AT1R-GFP, or HA-CXCR4 and treated with BFA at a concentration of 5 μg/ml for 8 h. The cell surface expression of α 2B -AR, β 2 -AR, and AT1R was determined by intact cell ligand binding using [ 3 H]RX 821002, [ 3 H]CGP-12177, and 125 I-Ang II, respectively, as described under Materials and Methods . The mean values of specific ligand binding were 22,737 ± 714, 17,718 ± 771, and 16,754 ± 782 ( n = 3, each in triplicate) from cells transfected with α 2B -AR, β 2 -AR, and AT1R, respectively. The cell surface expression of HA-CXCR4 was measured by flow cytometry after staining with anti-HA antibodies in unpermeabilized cells. The data shown are percentages of the mean value obtained from cells transfected with individual receptor and treated with ethanol (control) and are presented as the mean ± S.E. of three experiments. ∗, P

Techniques Used: Inhibition, Expressing, Transfection, Concentration Assay, Ligand Binding Assay, Flow Cytometry, Cytometry, Staining

5) Product Images from "Regulation of ?1- and ?3-adrenergic agonist-stimulated lipolytic response in hyperthyroid and hypothyroid rat white adipocytes"

Article Title: Regulation of ?1- and ?3-adrenergic agonist-stimulated lipolytic response in hyperthyroid and hypothyroid rat white adipocytes

Journal: British Journal of Pharmacology

doi: 10.1038/sj.bjp.0703008

Effect of thyroid status on [3 H]CGP 12177 binding sites
Figure Legend Snippet: Effect of thyroid status on [3 H]CGP 12177 binding sites

Techniques Used: Binding Assay

Concentration-response curves for stimulation of glycerol release from hyperthyroid (□), euthyroid control (Δ) and hypothyroid (○) rats, elicited by the partial agonists, the β 3 -selective agonist CGP 12177 (a) and the β 1 -selective agonist xamoterol (b). Each curve is a representative experiment performed in triplicate. Each point is the mean±s.e.mean over basal lipolysis value. Standard deviations not shown are within the symbol.
Figure Legend Snippet: Concentration-response curves for stimulation of glycerol release from hyperthyroid (□), euthyroid control (Δ) and hypothyroid (○) rats, elicited by the partial agonists, the β 3 -selective agonist CGP 12177 (a) and the β 1 -selective agonist xamoterol (b). Each curve is a representative experiment performed in triplicate. Each point is the mean±s.e.mean over basal lipolysis value. Standard deviations not shown are within the symbol.

Techniques Used: Concentration Assay

Related Articles

Amplified Luminescent Proximity Homogenous Assay:

Article Title: Impact of Polymorphic Variants on the Molecular Pharmacology of the Two-Agonist Conformations of the Human ?1-Adrenoceptor
Article Snippet: 3 H-CGP 12177, 3 H-adenine, 14 C-cAMP and 3 H-myo-inositol were from Amersham International (Buckinghamshire, UK). .. The Surefire Alphascreen pERK1/2 kit was obtained from PerkinElmer.

Synthesized:

Article Title: Investigation of the effect of the farnesyl protein transferase inhibitor R115777 on isoprenylation and intracellular signalling by the prostacyclin receptor
Article Snippet: Iloprost, [3 H]iloprost (15.3 Ci mmol−1 ), [3 H]-CGP-12177 (41.0 Ci mmol−1 ) and polyvinylidene difluoride (PVDF) filters were purchased from Amersham Pharmacia Biotech, Buckinghampshire, U.K. [3 H]mevalonolactone (20 Ci mmol−1 ), [3 H]farnesylpyrophosphate (FPP) (20 Ci mmol−1 ), [3 H]geranylgeranylpyrophosphate (GGPP) (15–30 Ci mmol−1 ), [35 S]methionine (1175 Ci mmol−1 ; 10 mC ml−1 ) and [3 H]cAMP (15–30 Ci mmol−1 ) were purchased from American Radiolabeled Chemicals Inc. Isoproterenol was purchased from Sigma, MO, U.S.A. Fura 2/AM and U46619 were purchased from Calbiochem, Darmstadt, Germany. .. Mouse monoclonal 101R anti -HA antibody was obtained from BabCO, Berkeley, U.S.A. Anti -HDJ-2 antibody was from Neomarkers, CA, U.S.A. Oligonucleotides were synthesized by Sigma Genosys Biotechnologies, St Louis, MO, U.S.A.

Purification:

Article Title: Effect of the statin atorvastatin on intracellular signalling by the prostacyclin receptor in vitro and in vivo
Article Snippet: Iloprost, [3 H]iloprost (15.3 Ci mmol−1 ) and [3 H]CGP-12177 (41.0 Ci mmol−1 ) were purchased from Amersham Pharmacia Biotech, Buckinghampshire, U.K. [3 H]adenosine 3′,5′-cyclic monophosphate (cAMP) (15–30 Ci mmol−1 ) was purchased from American Radiolabeled Chemicals Inc., St Louis, U.S.A. Isoproterenol was purchased from Sigma, St Louis, Missouri, U.S.A. Fura 2/AM St Louis, U.S.A. and U46619 were purchased from Calbiochem, Darmstadt, Germany. .. All other reagents were ANALAR or molecular biology grade and were used without further purification.

other:

Article Title: The effects of the statins lovastatin and cerivastatin on signalling by the prostanoid IP-receptor
Article Snippet: Iloprost, [3 H]-iloprost (15.3 Ci mmol−1 ) and [3 H]-CGP-12177 (41.0 Ci mmol−1 ) were purchased from Amersham Pharmacia Biotech.

Article Title: Predicting in vivo cardiovascular properties of ?-blockers from cellular assays: a quantitative comparison of cellular and cardiovascular pharmacological responses
Article Snippet: 3 H-CGP 12177, 3 H-adenine, and 14 C-cAMP were obtained from Amersham International (Little Chalfont, UK).

Activity Assay:

Article Title: ADP-Ribosylation Factors Modulate the Cell Surface Transport of G Protein-Coupled Receptors S⃞
Article Snippet: .. [3 H]CGP-12177 (specific activity = 51 Ci/mmol), [3 H]RX 821002 (41 Ci/mmol), l -[ N -methyl-3 H]scopolamine methyl chloride ([3 H]NMS, 80 Ci/mmol), and (3-(125 I)-iodotyrosyl 4) Ang II (125 I-Ang II) (2000 Ci/mmol) were purchased from GE Healthcare (Piscataway, NJ). .. Alexa Fluor 594-labeled secondary antibodies and 4,6-diamidino-2-phenylindole were from Invitrogen.

Article Title: Regulation of ?1- and ?3-adrenergic agonist-stimulated lipolytic response in hyperthyroid and hypothyroid rat white adipocytes
Article Snippet: .. [3 H]-CGP 12177 (specific activity: 46 Ci mmol−1 ) [α-32 P]-ATP (specific activity: 30 Ci mmol−1 ) and [α-32 P]-dCTP (specific activity: 3000 Ci mmol−1 ) were obtained from Amersham (Les Ulis, France). .. The binding characteristics are shown in .

Western Blot:

Article Title: Investigation of the effect of the farnesyl protein transferase inhibitor R115777 on isoprenylation and intracellular signalling by the prostacyclin receptor
Article Snippet: Iloprost, [3 H]iloprost (15.3 Ci mmol−1 ), [3 H]-CGP-12177 (41.0 Ci mmol−1 ) and polyvinylidene difluoride (PVDF) filters were purchased from Amersham Pharmacia Biotech, Buckinghampshire, U.K. [3 H]mevalonolactone (20 Ci mmol−1 ), [3 H]farnesylpyrophosphate (FPP) (20 Ci mmol−1 ), [3 H]geranylgeranylpyrophosphate (GGPP) (15–30 Ci mmol−1 ), [35 S]methionine (1175 Ci mmol−1 ; 10 mC ml−1 ) and [3 H]cAMP (15–30 Ci mmol−1 ) were purchased from American Radiolabeled Chemicals Inc. Isoproterenol was purchased from Sigma, MO, U.S.A. Fura 2/AM and U46619 were purchased from Calbiochem, Darmstadt, Germany. .. Rabbit reticulocyte translation system (minus methionine), T7 RNA polymerase, RNasin and all restriction endonucleases were purchased from Promega Corp., Madison, U.S.A. Taq DNA polymerase, the chemiluminescence Western blot detection kit and rat monoclonal 3F10 anti -haemagglutinin (HA) peroxidase-conjugated antibody were purchased from Roche, East Sussex, U.K. Horseradish peroxidase-conjugated goat anti -mouse IgG was from Santa Cruz Biotechnology, CA, U.S.A.

Article Title: The effect of the farnesyl protein transferase inhibitor SCH66336 on isoprenylation and signalling by the prostacyclin receptor
Article Snippet: Iloprost, [3 H]iloprost (15.3 Ci·mmol−1 ), [3 H]CGP-12177 (41.0 Ci·mmol−1 ) and PVDF filters were purchased from Amersham Biosciences. .. Rabbit reticulocyte translation system (minus methionine), T7 RNA polymerase, RNasin and all restriction endonucleases were purchased from Promega Corp. Taq DNA polymerase, the chemiluminescence Western detection kit, and rat monoclonal 3F10 anti-HA (haemagglutinin) peroxidase-conjugated antibody were purchased from Roche.

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    GE Healthcare h cgp 12177
    Inhibition of the cell surface expression of α 2B -AR, β 2 -AR, AT1R, and CXCR4 by BFA treatment. A, the cell surface expression of the receptors in cells treated with BFA. HEK293 cells were transfected with α 2B -AR-GFP, β 2 -AR-GFP, AT1R-GFP, or HA-CXCR4 and treated with BFA at a concentration of 5 μg/ml for 8 h. The cell surface expression of α 2B -AR, β 2 -AR, and AT1R was determined by intact cell ligand binding using [ 3 H]RX 821002, [ 3 <t>H]CGP-12177,</t> and 125 I-Ang II, respectively, as described under Materials and Methods . The mean values of specific ligand binding were 22,737 ± 714, 17,718 ± 771, and 16,754 ± 782 ( n = 3, each in triplicate) from cells transfected with α 2B -AR, β 2 -AR, and AT1R, respectively. The cell surface expression of HA-CXCR4 was measured by flow cytometry after staining with anti-HA antibodies in unpermeabilized cells. The data shown are percentages of the mean value obtained from cells transfected with individual receptor and treated with ethanol (control) and are presented as the mean ± S.E. of three experiments. ∗, P
    H Cgp 12177, supplied by GE Healthcare, used in various techniques. Bioz Stars score: 86/100, based on 2 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/result/h cgp 12177/product/GE Healthcare
    Average 86 stars, based on 2 article reviews
    Price from $9.99 to $1999.99
    h cgp 12177 - by Bioz Stars, 2020-04
    86/100 stars
      Buy from Supplier

    86
    GE Healthcare cgp 12177
    [ 3 <t>H]-CGP-12177</t> competition binding curves. These curves show the ability of ICI-118,551 (A), 5731869 (B), JB-143 (C) and JB-176 (D) to concentration-dependently displace [ 3 H]-CGP-12177 binding to β 1 - and β 2 -adrenoceptors. The curves are
    Cgp 12177, supplied by GE Healthcare, used in various techniques. Bioz Stars score: 86/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/result/cgp 12177/product/GE Healthcare
    Average 86 stars, based on 1 article reviews
    Price from $9.99 to $1999.99
    cgp 12177 - by Bioz Stars, 2020-04
    86/100 stars
      Buy from Supplier

    Image Search Results


    Inhibition of the cell surface expression of α 2B -AR, β 2 -AR, AT1R, and CXCR4 by BFA treatment. A, the cell surface expression of the receptors in cells treated with BFA. HEK293 cells were transfected with α 2B -AR-GFP, β 2 -AR-GFP, AT1R-GFP, or HA-CXCR4 and treated with BFA at a concentration of 5 μg/ml for 8 h. The cell surface expression of α 2B -AR, β 2 -AR, and AT1R was determined by intact cell ligand binding using [ 3 H]RX 821002, [ 3 H]CGP-12177, and 125 I-Ang II, respectively, as described under Materials and Methods . The mean values of specific ligand binding were 22,737 ± 714, 17,718 ± 771, and 16,754 ± 782 ( n = 3, each in triplicate) from cells transfected with α 2B -AR, β 2 -AR, and AT1R, respectively. The cell surface expression of HA-CXCR4 was measured by flow cytometry after staining with anti-HA antibodies in unpermeabilized cells. The data shown are percentages of the mean value obtained from cells transfected with individual receptor and treated with ethanol (control) and are presented as the mean ± S.E. of three experiments. ∗, P

    Journal: The Journal of Pharmacology and Experimental Therapeutics

    Article Title: ADP-Ribosylation Factors Modulate the Cell Surface Transport of G Protein-Coupled Receptors S⃞

    doi: 10.1124/jpet.109.161489

    Figure Lengend Snippet: Inhibition of the cell surface expression of α 2B -AR, β 2 -AR, AT1R, and CXCR4 by BFA treatment. A, the cell surface expression of the receptors in cells treated with BFA. HEK293 cells were transfected with α 2B -AR-GFP, β 2 -AR-GFP, AT1R-GFP, or HA-CXCR4 and treated with BFA at a concentration of 5 μg/ml for 8 h. The cell surface expression of α 2B -AR, β 2 -AR, and AT1R was determined by intact cell ligand binding using [ 3 H]RX 821002, [ 3 H]CGP-12177, and 125 I-Ang II, respectively, as described under Materials and Methods . The mean values of specific ligand binding were 22,737 ± 714, 17,718 ± 771, and 16,754 ± 782 ( n = 3, each in triplicate) from cells transfected with α 2B -AR, β 2 -AR, and AT1R, respectively. The cell surface expression of HA-CXCR4 was measured by flow cytometry after staining with anti-HA antibodies in unpermeabilized cells. The data shown are percentages of the mean value obtained from cells transfected with individual receptor and treated with ethanol (control) and are presented as the mean ± S.E. of three experiments. ∗, P

    Article Snippet: [3 H]CGP-12177 (specific activity = 51 Ci/mmol), [3 H]RX 821002 (41 Ci/mmol), l -[ N -methyl-3 H]scopolamine methyl chloride ([3 H]NMS, 80 Ci/mmol), and (3-(125 I)-iodotyrosyl 4) Ang II (125 I-Ang II) (2000 Ci/mmol) were purchased from GE Healthcare (Piscataway, NJ).

    Techniques: Inhibition, Expressing, Transfection, Concentration Assay, Ligand Binding Assay, Flow Cytometry, Cytometry, Staining

    [ 3 H]-CGP-12177 competition binding curves. These curves show the ability of ICI-118,551 (A), 5731869 (B), JB-143 (C) and JB-176 (D) to concentration-dependently displace [ 3 H]-CGP-12177 binding to β 1 - and β 2 -adrenoceptors. The curves are

    Journal: British Journal of Pharmacology

    Article Title: The design, synthesis and pharmacological characterization of novel ?2-adrenoceptor antagonists

    doi: 10.1111/j.1476-5381.2011.01269.x

    Figure Lengend Snippet: [ 3 H]-CGP-12177 competition binding curves. These curves show the ability of ICI-118,551 (A), 5731869 (B), JB-143 (C) and JB-176 (D) to concentration-dependently displace [ 3 H]-CGP-12177 binding to β 1 - and β 2 -adrenoceptors. The curves are

    Article Snippet: Saturation binding analyses of the two cell lines was conducted (see , n = 3 in triplicate) to provide K d values for [3 H]-CGP-12177 at the β1 -adrenoceptor (0.28 ± 0.16 nM) and β2 -adrenoceptor (0.15 ± 0.02 nM) expressing cell lines for use in the Cheng–Prusoff equation.

    Techniques: Binding Assay, Concentration Assay